右旋糖酐及羟丙甲基纤维素对层状复合氢氧化物-阿司匹林体系缓释性能的影响  

Effects of Dextran and HPMC on Sustained-Release Property of LDH-Acetosalicylic Acid System

作　　者：焦林[1] 苟国敬[1,2] 杨建宏[2] 杨晓萍[3] 朱彦殊[1] 闫乾顺[1] 刘建平[1] 李江[1] 

机构地区：[1]宁夏医科大学基础医学院,银川750004 [2]宁夏医科大学中医药现代化技术中心,银川750004 [3]宁夏医科大学高等卫生职业技术学院,银川750004

出　　处：《中国药学杂志》2011年第5期357-363,共7页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金(20961008);宁夏自然科学基金(NZ09102);宁夏高等学校科学技术研究重点项目基金(200919341);教育部科学技术研究重点项目基金资助(207127)

摘　　要：目的以阿司匹林(ASA)作层状复合氢氧化物(LDH)的插层客体,制备右旋糖酐(DET)修饰的LDH-ASA载药体系、评价羟丙甲基纤维素(HPMC)作辅料HPMC-DET-LDH-ASA制剂的药物释放性能,考察DET复合及HPMC等辅料对LDH载药系统缓释性能的影响及LDH用作药物载体的制剂效果。方法以DET-LDH-ASA三级超分子为载药体,HPMC等作辅助骨架材料,用粉末直接压片法压制HPMC-DET-LDH-ASA片剂,用紫外分光光度法测定不同介质中的药物释放度。结果相同介质中HPMC-DET-LDH-ASA制剂的缓释性优于LDH-ASA的HPMC骨架片,而HPMC-LDH-ASA骨架片的缓释性优于ASA的HPMC骨架片;HPMC-DET-LDH-ASA制剂在不同环境表现不同缓释效果与释放机制,在pH1.0的盐酸释放介质中形成不溶性凝胶骨架,药物从水化凝胶层向外扩散,持续12 h以上,在蒸馏水和pH6.8的磷酸盐释放介质中,药物通过溶蚀机制释放,持续时间小于6 h。结论 DET复合及HPMC等辅料的加入能显著提高LDH-ASA载药体系酸性环境下的缓释性能。OBJECTIVE Using acetylsalicylic acid（ASA） as the intercalated guest of layered double hydroxide（LDH）,and hydroxy-propyl-methylcellulose（HPMC） as the excipient,to prepare a drug-loading system modified by dressing agent,dextran（DET）.To evaluate the release property of the HPMC-DET-LDH-ASA sustained release tablet,and to study the effects of DET and HPMC on the release of the LDH-ASA system and investigate the utility of LDH as a drug carrier in matrix tablets.METHODS The sustained-release tablets were made by the direct powder compression method using DET-LDH-ASA super-molecule as the main body and HPMCK15M as matrix material.Drug dissolution in different media was measured by ultraviolet spectro-photometric method.RESULTS In the same medium,HPMC-DET-LDH-ASA tablet showed the best sustained-release effect,followed by HPMC-LDH-ASA tablet and then ASA original drug matrix tablet.The HPMC-DET-LDH-ASA sustained release tablets had different release behaviors with different mechanisms in different media： in hydrochloric acid medium with a pH of 1.0,the drug spread outward from the non-dissolution gel hydrated layer formed in matrix for more than 12 h.However,in distilled water or phosphate medium with pH 6.8,the drug released through corrosion mechanism with releasing time less than 6 h.CONCLUSION In acidic medium,the sustainede release of the LDH-ASA drug delivery system could be improved significantly by modification with DET and HPMC.

关 键 词：层状复合氢氧化物 阿司匹林 右旋糖酐 羟丙甲基纤维素 

分 类 号：R969[医药卫生—药理学] R979.1[医药卫生—药学]